Alesse 0.10 mg + 0.02 mg Tablets

Brand Name

The medication is marketed under the brand name Alesse, a widely recognized designation in the field of reproductive health and hormonal contraception.

International Nonproprietary Name (INN)

The active components in this product are identified internationally as ethinyl estradiol and levonorgestrel, names standardized for consistency across global pharmacological practices.

Form of Release

Alesse is available as film-coated tablets, designed for oral administration. These tablets are typically supplied in 28-day blister packs, containing 21 active tablets and 7 placebo tablets, facilitating a continuous daily dosing schedule.

Composition

Each active tablet of Alesse contains 0.02 mg of ethinyl estradiol and 0.1 mg of levonorgestrel as the primary hormonal agents. The formulation includes several inactive ingredients, such as lactose monohydrate, which serves as a filler, and microcrystalline cellulose, providing structural integrity. Additional excipients like magnesium stearate act as lubricants, while the film coating comprises hypromellose, titanium dioxide, and polyethylene glycol, often colored with iron oxides to distinguish active from placebo tablets. The placebo tablets contain no hormones but include similar inactive components to maintain consistency in appearance and administration.

Pharmacologic Properties

Pharmacodynamics

Alesse functions as a combined oral contraceptive, leveraging the synergistic effects of ethinyl estradiol and levonorgestrel to prevent ovulation. The ethinyl estradiol component, a synthetic estrogen, stabilizes the endometrial lining and suppresses follicle-stimulating hormone (FSH) release from the pituitary gland. Meanwhile, levonorgestrel, a progestin, inhibits luteinizing hormone (LH) secretion, preventing the mid-cycle LH surge required for egg release. Together, these actions create an inhospitable environment for conception by thickening cervical mucus, which impedes sperm penetration, and altering the endometrium to reduce the likelihood of implantation.

Beyond contraception, the hormonal blend regulates menstrual cycles, often reducing flow and cramping in women with irregular or heavy periods. The low-dose formulation minimizes systemic estrogen exposure compared to older contraceptives, balancing efficacy with a reduced risk of estrogen-related effects. Clinical data demonstrate a high success rate in preventing pregnancy when taken consistently, with additional benefits like decreased acne or ovarian cyst formation in some users. This dual-hormone approach underpins its reliability as a daily contraceptive option.

Pharmacokinetics

Upon oral intake, Alesse components are absorbed rapidly from the gastrointestinal tract, with ethinyl estradiol reaching peak plasma levels within 1 to 2 hours and levonorgestrel within 1 hour. Food does not significantly affect absorption, allowing flexibility in timing. Both hormones exhibit high plasma protein binding—ethinyl estradiol at 95–97% (mostly to albumin) and levonorgestrel at 97–99% (to sex hormone-binding globulin and albumin)—limiting their free circulation to target tissues like the ovaries and uterus.

Metabolism occurs primarily in the liver, where ethinyl estradiol undergoes extensive first-pass metabolism via cytochrome P450 enzyme CYP3A4, forming sulfate and glucuronide conjugates. Levonorgestrel is also metabolized by CYP3A4 into hydroxylated derivatives, though it experiences less first-pass effect. The half-life of ethinyl estradiol is approximately 24 hours, while levonorgestrel’s is 24 to 36 hours, supporting once-daily dosing. Excretion is predominantly urinary for ethinyl estradiol metabolites and biliary for levonorgestrel metabolites, with elimination completed within days of discontinuation.

Indications for Use

Alesse is primarily indicated for the prevention of pregnancy in women seeking reliable contraception. It is suitable for those desiring a hormonal method with a predictable withdrawal bleed mimicking a natural menstrual cycle. The medication is also prescribed to manage irregular menstrual cycles, reducing variability in timing and flow, and to alleviate dysmenorrhea, or painful periods, by stabilizing hormonal fluctuations.

In some cases, healthcare providers may recommend it for secondary benefits, such as reducing acne severity or mitigating symptoms of premenstrual syndrome (PMS) linked to hormonal shifts. While not a primary treatment, it can decrease the incidence of functional ovarian cysts by suppressing ovulation. These applications make it a versatile option for reproductive-age women addressing both contraceptive and gynecological needs.

Contraindications

Alesse is contraindicated in women with a history of venous thromboembolism, such as deep vein thrombosis or pulmonary embolism, due to the increased clotting risk associated with estrogen. It is also prohibited in those with known or suspected breast cancer, endometrial cancer, or other estrogen-dependent malignancies, as hormonal stimulation could exacerbate these conditions.

Patients with severe liver disease, including tumors or acute viral hepatitis, should not use this therapy, given its hepatic metabolism. Uncontrolled hypertension, migraine with aura, and a history of stroke or myocardial infarction further preclude its use due to cardiovascular risks. Women over 35 who smoke heavily are advised against it, as the combination heightens thromboembolism likelihood. Hypersensitivity to ethinyl estradiol, levonorgestrel, or any tablet component, such as lactose, is another absolute restriction.

Method of Administration and Dosage

Administration Guidelines

The tablets should be taken orally, swallowed whole with water to ensure consistent delivery. They can be consumed with or without food, offering flexibility in daily routines. Taking them at the same time each day enhances efficacy, particularly for the 21 active tablets, followed by 7 placebo tablets to maintain the habit during the hormone-free interval.

Dosage for Adults and Children

For adult women of reproductive age, the standard regimen of Alesse involves one tablet daily for 28 days, starting with an active tablet on the first day of menstruation or the first Sunday after it begins, depending on the prescribed schedule. The cycle repeats without interruption, with each pack providing 21 days of hormonal tablets (0.02 mg ethinyl estradiol and 0.1 mg levonorgestrel) and 7 days of placebo. Adolescents post-menarche may use the same regimen under medical supervision, but pre-pubertal children are not candidates, as the drug targets ovulatory cycles.

Dose Adjustment in Specific Conditions

No dose adjustments are typically required for renal impairment, as kidney function plays a secondary role in clearance. In mild to moderate liver dysfunction, caution is advised due to metabolic reliance on the liver, but severe hepatic impairment contraindicates use entirely. Missed doses should be addressed promptly—taking the missed tablet as soon as remembered, even if it means two tablets in one day—though backup contraception may be needed if more than 24 hours lapse. Consistency is critical, and adjustments for specific conditions should be guided by a healthcare provider.

Side Effects

Alesse may cause a range of side effects, though many women experience only mild or transient reactions. Common issues include nausea, breast tenderness, or spotting between periods, particularly during the first few cycles as the body adjusts. Headaches and mood changes, such as irritability or mild depression, are also reported, often stabilizing with continued use.

Less frequent effects include weight gain, bloating, or changes in libido, tied to hormonal shifts. Serious but rare reactions, such as thromboembolism (e.g., leg pain or shortness of breath), liver dysfunction (e.g., jaundice), or severe hypertension, require immediate discontinuation and medical attention. Allergic responses, like rash or swelling, are uncommon but warrant cessation if significant. Regular check-ups help monitor these effects and ensure the therapy remains suitable.

Overdose

Symptoms of Overdose

Excessive intake of Alesse is unlikely to cause acute, life-threatening symptoms due to its low hormonal doses. Overdose reports suggest nausea, vomiting, and vaginal bleeding as primary manifestations, reflecting an exaggerated hormonal response. Severe outcomes are rare, but prolonged excess could theoretically amplify side effects like headache or fatigue.

First Aid Measures

In case of overdose, medical advice should be sought, though emergency measures are seldom needed. No specific antidote exists, so treatment focuses on symptom management, such as antiemetics for nausea or rest for discomfort. Monitoring is advised until symptoms resolve, typically within hours to days, given the drugs’ rapid clearance.

Drug Interactions

Effects on Other Medications

Alesse can be affected by drugs that induce cytochrome P450 enzymes, particularly CYP3A4, such as rifampin, phenytoin, or carbamazepine, which may accelerate metabolism and reduce contraceptive efficacy. This interaction necessitates backup contraception during and for 28 days after such co-administration. Conversely, inhibitors like ketoconazole might increase hormone levels, though this is rarely significant.

The medication may also elevate levels of drugs like cyclosporine by competing for metabolic pathways, requiring dose adjustments. Antibiotics like penicillin or tetracycline do not typically interfere, despite historical concerns, unless they induce enzymes indirectly. A full medication review with a healthcare provider ensures safe co-use.

Compatibility with Alcohol and Food

Moderate alcohol consumption does not diminish the drug’s effectiveness, allowing typical social use without concern. Food intake has minimal impact on absorption, so tablets can be taken with meals or on an empty stomach, accommodating individual preferences seamlessly.

Special Precautions

Use During Pregnancy and Breastfeeding

Alesse is contraindicated in pregnancy, as it is intended to prevent conception, and hormonal exposure could pose risks to fetal development if inadvertently continued. Women should discontinue use immediately if pregnancy is confirmed and consult a doctor. During breastfeeding, it is not recommended, especially in the first six weeks postpartum, as levonorgestrel may pass into milk and affect infant growth, while estrogen could reduce milk supply.

Non-hormonal contraception is preferred during lactation until breastfeeding stabilizes, after which low-dose progestin-only options may be considered if Alesse is unsuitable.

Impact on Driving and Operating Machinery

The medication does not typically impair cognitive or motor functions, making it safe for most women to drive or operate machinery. Rare instances of dizziness or fatigue suggest caution during initial use until personal response is established, particularly in the first cycle.

Considerations for Elderly and Pediatric Populations

Elderly women beyond reproductive age rarely use Alesse, as its contraceptive purpose becomes irrelevant post-menopause, and hormonal risks outweigh benefits. Adolescents post-menarche can use it effectively, with no significant differences in safety compared to adults, though pre-pubertal children are excluded due to lack of ovulatory cycles and untested safety in this group.